TABLE 1

Parameters for drug competition toward specific [3H]EBDN binding to hα 4β2-nAChR in transfected SH-EP1 cells

Radioligand binding competition assays were conducted as described under Materials and Methods and in the legend to Fig. 6. Results were fit to the logistic equation to determine log IC50 values (± S.E.M.), mean IC50 values, and Hill coefficients (± S.E.M.).

Drug log IC50 IC50nH
μM
Epibatidine −9.31 ± 0.04 0.00049 −0.98 ± 0.08
Cytisine −8.00 ± 0.03 0.010 −0.89 ± 0.05
Lobeline −7.12 ± 0.07 0.076 −0.58 ± 0.05
Nicotine −7.09 ± 0.05 0.081 −0.96 ± 0.09
Suberyldicholine −6.28 ± 0.03 0.52 −0.91 ± 0.05
ACh −6.13 ± 0.02 0.74 −0.92 ± 0.03
DMPP −6.08 ± 0.05 0.83 −0.97 ± 0.09
DHβE −5.46 ± 0.06 3.5 −0.81 ± 0.07
Carbamylcholine −5.22 ± 0.03 6.0 −0.97 ± 0.06
Acetylthiocholine −5.15 ± 0.03 7.1 −1.06 ± 0.08
Decamethonium −4.28 ± 0.04 52 −0.77 ± 0.05
d-Tubocurarine −4.09 ± 0.09 81 −0.73 ± 0.06
MLA −4.02 ± 0.03 95 −0.57 ± 0.03
Succinylcholine −3.92 ± 0.04 120 −0.76 ± 0.06
Choline −3.54 ± 0.04 290 −0.84 ± 0.07
Alcuronium −3.12 ± 0.11 760 −0.59 ± 0.11
Vecuronium −3.01 ± 0.06 980 −0.69 ± 0.08
Hexamethonium −2.73 ± 0.15 1,900 −1.13 ± 0.34
Pancuronium −2.63 ± 0.11 2,300 −0.82 ± 0.14
Mecamylamine ≪-4 ≫100
Eserine <-3 >1,000